US4968494AExpiredUtility

Methods and compositions for thrombolytic therapy

47
Assignee: MERCK & CO INCPriority: Mar 27, 1987Filed: Apr 10, 1990Granted: Nov 6, 1990
Est. expiryMar 27, 2007(expired)· nominal 20-yr term from priority
A61K 31/415A61K 31/335A61K 31/41A61K 31/42A61K 31/425A61K 31/445A61K 31/535A61K 38/166A61K 38/49
47
PatentIndex Score
12
Cited by
4
References
10
Claims

Abstract

Certain Factor XIIIa inhibitor compounds have been discovered which have been found to be useful in the lysis of blood clots and thus adaptable for administration in thrombolytic therapy either alone or together with plasminogen activator.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A composition suitable for thrombolytic or fibrinolytic therapy comprising a therapeutic amount of a Factor XIIIa inhibitor compound in a pharmaceutically acceptable carrier wherein the factor XIIIa inhibitor compound is 2-(1-acetonylthio)-5-methylthiazolo(2,3-b)-1,3,4-thiadiazolium perchlorate. 
     
     
       2. A composition according to claim 1 wherein the pharmaceutically acceptable carrier is a sterile physiological medium. 
     
     
       3. A composition according to claim 1 which also contains a plasminogen activator. 
     
     
       4. A method for lysing clots in thrombotic patients which comprises intravenously administering a therapeutically effective amount of a composition comprising a Factor XIIIa inhibitor compound, said Factor XIIIa inhibitor compound being 2-(1-acetonylthio)-5-methyl-thiazolo(2,3,-b)-1,3,4-thiadiazolium perchlorate. 
     
     
       5. A method according to claim 4 wherein a plasminogen activator is also administered. 
     
     
       6. A method according to claim 5 wherein the plasminogen activator is tissue plasminogen activator. 
     
     
       7. A method according to claim 5 wherein the plasminogen activator is selected from the group consisting of tissue plasminogen activator, urokinase, prourokinase, streptokinase and eminase. 
     
     
       8. A method according to claim 4 wherein the therapeutic dose is delivered by a single, multiple or continuous intravenous administration. 
     
     
       9. A method according to claim 8 wherein the therapeutic dose is delivered by continuous infusion. 
     
     
       10. A method according to claim 4 wherein the Factor XIIIa inhibitor compound is administered first in a single bolus and the plasmingen activator then administered by continuous infusion.

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